Sotorasib (AMG510) is a highly selective targeted drug for the KRASG12C mutation. Developed by Amgen Inc., it received accelerated approval from the U.S. FDA in 2021 for the treatment of non-small cell lung cancer (NSCLC).
What is Sotorasib (AMG510)?
Sotorasib (AMG510) is a highly selective targeted drug for the KRASG12C mutation. It covalently binds to the mutant cysteine residue of the KRASG12C protein, locking it in an inactive state and inhibiting the downstream MAPK signaling pathway, thereby blocking tumor cell proliferation and inducing apoptosis.
Dosage Forms, Strengths and Properties of Sotorasib (AMG510)
Drug Components and Dosage Forms
Active Ingredient: Each tablet contains 120 mg of sotorasib (equivalent to the free base form), present as the sulfate salt.
Excipients: Microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, etc. The film coating contains polyvinyl alcohol, titanium dioxide, polyethylene glycol, etc.
Appearance and Strengths
Dosage Form: Yellow, oval-shaped film-coated tablets, engraved with "AMG" on one side and "120" on the other side.
120 tablets per bottle (NDC 55513-488-02)
240 tablets per bottle (NDC 55513-488-24)
Storage Conditions
Store at room temperature between 20°C and 25°C (68°F and 77°F). Short-term storage between 15°C and 30°C (59°F and 86°F) is permitted.
Dosage and Administration of Sotorasib (AMG510)
Recommended Dosage
Standard Dosage: 960 mg (8 tablets of 120 mg each) taken orally once daily, until disease progression or unacceptable toxicity occurs.
Administration Method
Swallow the tablets whole; do not chew, split, or crush them.
It can be taken with or without food (food may increase the AUC by 25%).
For dispersion administration (if needed): Add the tablets to 120 mL of non-carbonated water, stir to form small particles, and drink immediately. Complete the entire dose within 2 hours, and rinse the container with another 120 mL of water and drink the rinsing water.
Dose Adjustment
Hepatotoxicity: If AST/ALT levels are Grade ≥ 3 or accompanied by elevated bilirubin, suspend administration. After recovery, reduce the dose to 480 mg or 240 mg once daily.
ILD/Pneumonitis: Discontinue administration immediately in suspected cases; permanently discontinue the drug upon confirmation of diagnosis.
Other Grade 3-4 Adverse Reactions: Such as diarrhea, nausea, vomiting, etc., suspend administration until the adverse reaction is reduced to Grade ≤ 1, then resume treatment with a reduced dose.
Drug Interactions
Avoid concurrent use with PPIs/H2 receptor antagonists. If necessary, administer the drugs at intervals: take sotorasib 4 hours apart from antacids or 10 hours apart from H2 antagonists.
Avoid concurrent use with strong CYP3A4 inducers (e.g., rifampicin) and sensitive CYP3A4/P-gp substrates (e.g., midazolam, digoxin).
Missed Dose Management: If a dose is missed by more than 6 hours, skip the missed dose and take the next dose as scheduled the following day.
